WO2014043706A8 - Procédé de synthèse d'analogues de l'hormone thyroïdienne et de ses polymorphes - Google Patents

Procédé de synthèse d'analogues de l'hormone thyroïdienne et de ses polymorphes Download PDF

Info

Publication number
WO2014043706A8
WO2014043706A8 PCT/US2013/060177 US2013060177W WO2014043706A8 WO 2014043706 A8 WO2014043706 A8 WO 2014043706A8 US 2013060177 W US2013060177 W US 2013060177W WO 2014043706 A8 WO2014043706 A8 WO 2014043706A8
Authority
WO
WIPO (PCT)
Prior art keywords
thyroid hormone
compounds
hormone analogs
polymorphs
pyridazinone
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Ceased
Application number
PCT/US2013/060177
Other languages
English (en)
Other versions
WO2014043706A1 (fr
Inventor
D. Keith HESTER II
Robert J. Duguid
Martha Kelly
Anna CHASNOFF
Gang Dong
Edwin L. CROW
Rebecca Taub
Charles H. Reynolds
Duk Soon CHOI
Lianhe Shu
Ping Wang
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
F Hoffmann La Roche AG
Madrigal Pharmaceuticals Inc
Original Assignee
F Hoffmann La Roche AG
Madrigal Pharmaceuticals Inc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Priority to ES13837402T priority Critical patent/ES2795450T3/es
Priority to MX2015003418A priority patent/MX364661B/es
Priority to EP21209827.1A priority patent/EP4023641B1/fr
Priority to HK16100496.1A priority patent/HK1212682B/en
Priority to BR112015005891A priority patent/BR112015005891A2/pt
Priority to EP20157696.4A priority patent/EP3689853B1/fr
Priority to AU2013315017A priority patent/AU2013315017C1/en
Priority to IN3133DEN2015 priority patent/IN2015DN03133A/en
Priority to IL314360A priority patent/IL314360B2/en
Priority to EP13837402.0A priority patent/EP2895466B1/fr
Priority to IL320269A priority patent/IL320269A/en
Priority to IL288133A priority patent/IL288133B2/en
Priority to MYPI2015000591A priority patent/MY170520A/en
Priority to DK13837402.0T priority patent/DK2895466T3/da
Priority to NZ705827A priority patent/NZ705827A/en
Priority to EP24173563.8A priority patent/EP4406594B1/fr
Priority to CA2884481A priority patent/CA2884481C/fr
Priority to EP25200792.7A priority patent/EP4691557A3/fr
Priority to KR1020187034908A priority patent/KR102138750B1/ko
Priority to JP2015532148A priority patent/JP6616688B2/ja
Priority to RU2015114327A priority patent/RU2668960C2/ru
Priority to KR1020207005528A priority patent/KR20200023528A/ko
Priority to KR1020157009807A priority patent/KR101966490B1/ko
Priority to CN201380059943.5A priority patent/CN105008335B/zh
Priority to KR1020217019940A priority patent/KR102363776B1/ko
Priority to SG11201501907YA priority patent/SG11201501907YA/en
Application filed by F Hoffmann La Roche AG, Madrigal Pharmaceuticals Inc filed Critical F Hoffmann La Roche AG
Priority to BR122021024202-0A priority patent/BR122021024202B1/pt
Priority to MX2018014924A priority patent/MX395148B/es
Publication of WO2014043706A1 publication Critical patent/WO2014043706A1/fr
Priority to IL237628A priority patent/IL237628B/en
Priority to ZA2015/01795A priority patent/ZA201501795B/en
Priority to US14/660,720 priority patent/US9266861B2/en
Anticipated expiration legal-status Critical
Priority to US15/046,213 priority patent/US9968612B2/en
Publication of WO2014043706A8 publication Critical patent/WO2014043706A8/fr
Priority to US15/949,389 priority patent/US10376517B2/en
Priority to IL259610A priority patent/IL259610B/en
Priority to IL265030A priority patent/IL265030B/en
Priority to US16/458,546 priority patent/US10894050B2/en
Priority to IL275393A priority patent/IL275393B/en
Priority to US17/118,706 priority patent/US11564926B2/en
Priority to US18/066,677 priority patent/US20230210856A1/en
Priority to US18/393,813 priority patent/US11986481B2/en
Priority to US18/393,818 priority patent/US20240148742A1/en
Priority to LTPA2026507C priority patent/LTPA2026507I1/lt
Priority to FR26C1009C priority patent/FR26C1009I1/fr
Priority to NL301369C priority patent/NL301369I2/nl
Ceased legal-status Critical Current

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D237/00Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings
    • C07D237/02Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings
    • C07D237/06Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
    • C07D237/10Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D237/14Oxygen atoms
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/50Pyridazines; Hydrogenated pyridazines
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/50Pyridazines; Hydrogenated pyridazines
    • A61K31/501Pyridazines; Hydrogenated pyridazines not condensed and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/53Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/14Drugs for disorders of the endocrine system of the thyroid hormones, e.g. T3, T4
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D237/00Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings
    • C07D237/02Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings
    • C07D237/06Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
    • C07D237/10Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D237/14Oxygen atoms
    • C07D237/16Two oxygen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13Crystalline forms, e.g. polymorphs
    • YGENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02PCLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
    • Y02P20/00Technologies relating to chemical industry
    • Y02P20/50Improvements relating to the production of bulk chemicals
    • Y02P20/55Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Endocrinology (AREA)
  • Diabetes (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Peptides Or Proteins (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Medicinal Preparation (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Measuring Or Testing Involving Enzymes Or Micro-Organisms (AREA)
  • Steroid Compounds (AREA)

Abstract

La présente invention concerne des procédés de synthèse de composés pyridazinone utilisés comme analogues de l'hormone thyroïdienne et leurs promédicaments. De préférence, les procédés selon l'invention permettent de préparer à grande échelle des composés pyridazinone de pureté élevée. Dans certains modes de réalisation, les procédés selon l'invention permettent de préférence également de préparer des composés pyridazinone avec un rendement plus élevé que les procédés précédemment utilisés dans la préparation de tels composés. L'invention concerne également des formes polymorphes d'un composé pyridazinone. L'invention concerne en outre une méthode de traitement d'une résistance à une hormone thyroïdienne chez un sujet ayant au moins une mutation TRP.
PCT/US2013/060177 2012-09-17 2013-09-17 Procédé de synthèse d'analogues de l'hormone thyroïdienne et de ses polymorphes Ceased WO2014043706A1 (fr)

Priority Applications (44)

Application Number Priority Date Filing Date Title
KR1020217019940A KR102363776B1 (ko) 2012-09-17 2013-09-17 갑상선 호르몬 유사체 및 이의 다형의 합성 방법
EP21209827.1A EP4023641B1 (fr) 2012-09-17 2013-09-17 Procédé de synthèse d'analogues de l'hormone thyroïdienne et de ses polymorphes
HK16100496.1A HK1212682B (en) 2012-09-17 2013-09-17 Method of synthesizing thyroid hormone analogs and polymorphs thereof
BR112015005891A BR112015005891A2 (pt) 2012-09-17 2013-09-17 método de sintetizar análogos do hormônio da tireoide e polimorfos destes
EP20157696.4A EP3689853B1 (fr) 2012-09-17 2013-09-17 Procédé de synthèse d'analogues de l'hormone thyroïdienne et de ses polymorphes
AU2013315017A AU2013315017C1 (en) 2012-09-17 2013-09-17 Method of synthesizing thyroid hormone analogs and polymorphs thereof
IN3133DEN2015 IN2015DN03133A (fr) 2012-09-17 2013-09-17
IL314360A IL314360B2 (en) 2012-09-17 2013-09-17 Method for the synthesis of thyroid hormone analogs and their polymorphs
EP13837402.0A EP2895466B1 (fr) 2012-09-17 2013-09-17 Procédé de synthèse d'analogues de l'hormone thyroïdienne et de ses polymorphes
IL320269A IL320269A (en) 2012-09-17 2013-09-17 Method for the synthesis of thyroid hormone analogs and their polymorphs
IL288133A IL288133B2 (en) 2012-09-17 2013-09-17 Method of synthesizing thyroid hormone analogs and polymorphs thereof
MYPI2015000591A MY170520A (en) 2012-09-17 2013-09-17 Method of synthesizing thyroid hormone analogs and polymorphs thereof
DK13837402.0T DK2895466T3 (da) 2012-09-17 2013-09-17 Fremgangsmåde til syntese af thyreoideahormonanaloger og polymorfer deraf
NZ705827A NZ705827A (en) 2012-09-17 2013-09-17 Method of synthesizing thyroid hormone analogs and polymorphs thereof
EP24173563.8A EP4406594B1 (fr) 2012-09-17 2013-09-17 Analogues d'hormone thyroidienne
CA2884481A CA2884481C (fr) 2012-09-17 2013-09-17 Procede de synthese d'analogues de l'hormone thyroidienne et de ses polymorphes
EP25200792.7A EP4691557A3 (fr) 2012-09-17 2013-09-17 Procede de synthese d'analogues d'hormone thyroidienne et de polymorphes de ces analogues
KR1020187034908A KR102138750B1 (ko) 2012-09-17 2013-09-17 갑상선 호르몬 유사체 및 이의 다형의 합성 방법
MX2015003418A MX364661B (es) 2012-09-17 2013-09-17 Metodo para sintetizar los analogos de hormona tiroidea y leucocitos polimorfonucleares de los mismos.
RU2015114327A RU2668960C2 (ru) 2012-09-17 2013-09-17 Способ синтеза аналогов гормонов щитовидной железы и их полиморфов
KR1020207005528A KR20200023528A (ko) 2012-09-17 2013-09-17 갑상선 호르몬 유사체 및 이의 다형의 합성 방법
KR1020157009807A KR101966490B1 (ko) 2012-09-17 2013-09-17 갑상선 호르몬 유사체 및 이의 다형의 합성 방법
CN201380059943.5A CN105008335B (zh) 2012-09-17 2013-09-17 合成甲状腺激素类似物及其多形体的方法
ES13837402T ES2795450T3 (es) 2012-09-17 2013-09-17 Procedimiento para sintetizar análogos de hormonas tiroideas y polimorfos de los mismos
JP2015532148A JP6616688B2 (ja) 2012-09-17 2013-09-17 甲状腺ホルモンアナログ及びその多形体の合成方法
SG11201501907YA SG11201501907YA (en) 2012-09-17 2013-09-17 Method of synthesizing thyroid hormone analogs and polymorphs thereof
BR122021024202-0A BR122021024202B1 (pt) 2012-09-17 2013-09-17 Processo sintético compreendendo compostos de piridazinona bem como os ditos compostos
MX2018014924A MX395148B (es) 2012-09-17 2013-09-17 Método para sintetizar los análogos de hormona tiroidea y leucocitos polimorfonucleares de los mismos.
IL237628A IL237628B (en) 2012-09-17 2015-03-09 Method of synthesizing thyroid hormone analogs and polymorphs thereof
ZA2015/01795A ZA201501795B (en) 2012-09-17 2015-03-16 Method of synthesizing thyroid hormone analogs and polymorphs thereof
US14/660,720 US9266861B2 (en) 2012-09-17 2015-03-17 Method of synthesizing thyroid hormone analogs and polymorphs thereof
US15/046,213 US9968612B2 (en) 2012-09-17 2016-02-17 Method of synthesizing thyroid hormone analogs and polymorphs thereof
US15/949,389 US10376517B2 (en) 2012-09-17 2018-04-10 Methods of synthesizing thyroid hormone analogs and polymorphs thereof
IL259610A IL259610B (en) 2012-09-17 2018-05-27 Method of synthesizing thyroid hormone analogs and polymorphs thereof
IL265030A IL265030B (en) 2012-09-17 2019-02-25 Method of synthesizing thyroid hormone analogs and polymorphs thereof
US16/458,546 US10894050B2 (en) 2012-09-17 2019-07-01 Methods of synthesizing thyroid hormone analogs and polymorphs thereof
IL275393A IL275393B (en) 2012-09-17 2020-06-15 A method for synthesizing thyroid hormone analogs and their polymorphs
US17/118,706 US11564926B2 (en) 2012-09-17 2020-12-11 Methods of synthesizing thyroid hormone analogs and polymorphs thereof
US18/066,677 US20230210856A1 (en) 2012-09-17 2022-12-15 Methods of synthesizing thyroid hormone analogs and polymorphs thereof
US18/393,813 US11986481B2 (en) 2012-09-17 2023-12-22 Method of synthesizing thyroid hormone analogs and polymorphs thereof
US18/393,818 US20240148742A1 (en) 2012-09-17 2023-12-22 Method of synthesizing thyroid hormone analogs and polymorphs thereof
LTPA2026507C LTPA2026507I1 (fr) 2012-09-17 2026-02-20
FR26C1009C FR26C1009I1 (fr) 2012-09-17 2026-02-26 Analogues d'hormone thyroidienne
NL301369C NL301369I2 (nl) 2012-09-17 2026-03-02 resmetirom of een farmaceutisch aanvaardbaar zout daarvan

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US201261702137P 2012-09-17 2012-09-17
US61/702,137 2012-09-17
US201361790432P 2013-03-15 2013-03-15
US61/790,432 2013-03-15

Related Child Applications (1)

Application Number Title Priority Date Filing Date
US14/660,720 Continuation US9266861B2 (en) 2012-09-17 2015-03-17 Method of synthesizing thyroid hormone analogs and polymorphs thereof

Publications (2)

Publication Number Publication Date
WO2014043706A1 WO2014043706A1 (fr) 2014-03-20
WO2014043706A8 true WO2014043706A8 (fr) 2017-10-19

Family

ID=50278769

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2013/060177 Ceased WO2014043706A1 (fr) 2012-09-17 2013-09-17 Procédé de synthèse d'analogues de l'hormone thyroïdienne et de ses polymorphes

Country Status (31)

Country Link
US (8) US9266861B2 (fr)
EP (5) EP3689853B1 (fr)
JP (8) JP6616688B2 (fr)
KR (4) KR102363776B1 (fr)
CN (2) CN105008335B (fr)
AR (1) AR092872A1 (fr)
AU (1) AU2013315017C1 (fr)
BR (2) BR122021024202B1 (fr)
CA (3) CA2884481C (fr)
DK (3) DK4406594T3 (fr)
ES (3) ES2795450T3 (fr)
FI (2) FI4406594T3 (fr)
FR (1) FR26C1009I1 (fr)
HR (1) HRP20251398T1 (fr)
IL (7) IL314360B2 (fr)
IN (1) IN2015DN03133A (fr)
LT (2) LT4406594T (fr)
MX (2) MX364661B (fr)
MY (1) MY170520A (fr)
NL (1) NL301369I2 (fr)
NO (1) NO2026010I1 (fr)
NZ (2) NZ739645A (fr)
PL (1) PL4406594T3 (fr)
PT (1) PT4406594T (fr)
RS (1) RS67728B1 (fr)
RU (2) RU2668960C2 (fr)
SG (3) SG10202006058QA (fr)
SI (1) SI4406594T1 (fr)
TW (4) TWI681957B (fr)
WO (1) WO2014043706A1 (fr)
ZA (1) ZA201501795B (fr)

Families Citing this family (47)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AR092872A1 (es) 2012-09-17 2015-05-06 Madrigal Pharmaceuticals Inc Metodo para sintetizar analogos de la hormona tiroidea y polimorfos de los mismos
WO2018075650A1 (fr) 2016-10-18 2018-04-26 Madrigal Pharmaceuticals, Inc. Méthodes de traitement de troubles hépatiques ou de troubles lipidiques avec un agoniste thr-bêta
JP7156722B2 (ja) * 2018-01-23 2022-10-19 深▲チェン▼市塔吉瑞生物医薬有限公司 置換ピリダジノン化合物
ES3029158T3 (en) 2018-06-12 2025-06-23 Xizang Haisco Pharmaceutical Co Ltd Thyroid hormone receptor agonists and uses thereof
CN110627773B (zh) * 2018-06-22 2021-03-19 海创药业股份有限公司 氘代mgl-3196化合物及其用途
AR115666A1 (es) * 2018-07-02 2021-02-10 Madrigal Pharmaceuticals Inc Formas sólidas de 2-(3,5-dicloro-4-((5-isopropil-6-oxo-1,6-dihidropiridazin-3-il)oxi)fenil)-3,5-dioxo-2,3,4,5-tetrahidro-1,2,4-triazin-6-carbonitrilo
CA3113373A1 (fr) * 2018-10-12 2020-04-16 InventisBio Co., Ltd. Agonistes du recepteur des hormones thyroidiennes
CN111320609A (zh) 2018-12-13 2020-06-23 拓臻股份有限公司 一种THRβ受体激动剂化合物及其制备方法和用途
CN113474335B (zh) * 2019-02-21 2024-12-03 南京瑞捷医药科技有限公司 化合物及其作为甲状腺激素受体激动剂的用途
KR20220017917A (ko) 2019-05-08 2022-02-14 알리고스 테라퓨틱스 인코포레이티드 Thr-베타의 조절제 및 이의 사용 방법
WO2020228577A1 (fr) * 2019-05-10 2020-11-19 深圳微芯生物科技股份有限公司 Dérivé de pyridazinone et son utilisation
WO2020239076A1 (fr) * 2019-05-29 2020-12-03 南京明德新药研发有限公司 DÉRIVÉS DE PYRIDAZINONE CONSTITUANT DES AGONISTES DU RÉCEPTEUR DE LA THYROXINE DE TYPE β ET LEUR UTILISATION
AU2020336272A1 (en) 2019-08-23 2022-04-14 Terns Pharmaceuticals, Inc. Thyroid hormone receptor beta agonist compounds
WO2021043185A1 (fr) * 2019-09-04 2021-03-11 Sunshine Lake Pharma Co., Ltd. Composé utilisé comme agoniste du récepteur bêta des hormones thyroïdiennes et son utilisation
WO2021050945A1 (fr) 2019-09-12 2021-03-18 Terns, Inc. Composés agonistes du récepteur bêta de l'hormone thyroïdienne
WO2021063367A1 (fr) * 2019-09-30 2021-04-08 苏州科睿思制药有限公司 Forme cristalline de resmetirom, son procédé de préparation et son utilisation
CN112707892A (zh) * 2019-10-24 2021-04-27 苏州泽璟生物制药股份有限公司 哒嗪酮或哒嗪类化合物及其衍生物和药物组合物
WO2021104288A1 (fr) 2019-11-26 2021-06-03 昆药集团股份有限公司 Composé de 1,2,4-triazine-3,5-dione, son procédé de préparation et son utilisation
TW202128668A (zh) * 2019-12-16 2021-08-01 大陸商江蘇恆瑞醫藥股份有限公司 并環類衍生物、其製備方法及其在醫藥上的應用
WO2021129465A1 (fr) * 2019-12-26 2021-07-01 苏州科睿思制药有限公司 Cristal de resmétirom, son procédé de préparation et ses utilisations
WO2022041026A1 (fr) * 2020-08-27 2022-03-03 InventisBio Co., Ltd. Composés de pyridazinone
WO2022052822A1 (fr) * 2020-09-10 2022-03-17 苏州科睿思制药有限公司 Forme cristalline de resmetirom, son procédé de préparation et son utilisation
EP4204419A1 (fr) 2020-10-19 2023-07-05 Teva Pharmaceuticals International GmbH Formes solides de resmetirom
CN114437042A (zh) * 2020-11-03 2022-05-06 深圳微芯生物科技股份有限公司 酞嗪类化合物的晶型及其制备方法
CN114437034A (zh) * 2020-11-06 2022-05-06 深圳微芯生物科技股份有限公司 一种酞嗪类化合物的可药用盐、晶型及其制备方法
KR20230142523A (ko) * 2021-02-01 2023-10-11 마드리갈 파마슈티칼스, 인크. 간 장애 또는 지질 장애의 치료를 위한 로수바스타틴 및 레스메티롬의 치료용 조합
CN114907327A (zh) * 2021-02-10 2022-08-16 杭州领业医药科技有限公司 Resmetirom的晶型及其制备方法和用途
CN115073429A (zh) * 2021-03-15 2022-09-20 昆药集团股份有限公司 一种1,2,4-三嗪-3,5-二酮类化合物的盐型、晶型及其制备方法
CN118251221A (zh) 2021-09-27 2024-06-25 马德里加尔制药公司 用于减少肝脏体积的瑞司美替罗
WO2024165571A2 (fr) 2023-02-06 2024-08-15 E-Therapeutics Plc Inhibiteurs d'expression et/ou de fonction
EP4568664B1 (fr) 2023-04-07 2026-04-01 Terns Pharmaceuticals, Inc. Combinaison comprenant un agoniste thr-beta et un agoniste glp-1r pour son utilisation dans le traitement de l'obésité
CN116768802B (zh) * 2023-05-25 2025-11-21 杭州科巢生物科技有限公司 一种瑞司美替罗的合成方法
WO2024263714A1 (fr) 2023-06-22 2024-12-26 Madrigal Pharmaceuticals, Inc. BIOMARQUEURS POUR LE TRAITEMENT DE TROUBLES HÉPATIQUES AVEC DES AGONISTES THR-β ET UTILISATIONS ASSOCIÉES
CN119613386A (zh) * 2023-09-14 2025-03-14 杭州科巢生物科技有限公司 一种瑞司美替罗1,4-二氧六环溶剂化合物及其制备方法
CN117263870B (zh) * 2023-09-21 2026-02-06 江西同和药业股份有限公司 一种Resmetirom关键中间体III的制备方法
WO2025083699A2 (fr) 2023-10-16 2025-04-24 Cipla Limited Polymorphes de resmétirom et procédé associé
WO2025125576A2 (fr) 2023-12-15 2025-06-19 E-Therapeutics Plc Inhibiteurs d'expression et/ou de fonction
WO2025133348A1 (fr) 2023-12-22 2025-06-26 E-Therapeutics Plc Inhibiteurs d'expression et/ou de fonction
EP4686757A1 (fr) 2024-07-31 2026-02-04 e-therapeutics PLC Inhibiteurs d expression et/ou de fonction
WO2025164161A1 (fr) * 2024-01-29 2025-08-07 シオノギファーマ株式会社 Solvate de cannabidiol et procédé de purification de cannabidiol
WO2025171032A1 (fr) 2024-02-06 2025-08-14 Madrigal Pharmaceuticals, Inc. Méthodes de traitement d'une stéatose hépatique
US12377104B1 (en) 2024-02-06 2025-08-05 Madrigal Pharmaceuticals, Inc. Methods for treating a fatty liver disease
WO2025191457A1 (fr) * 2024-03-13 2025-09-18 Morepen Laboratories Limited Procédé de préparation d'un dérivé de pyridazinone
CN119019375A (zh) * 2024-08-14 2024-11-26 奥锐特药业(天津)有限公司 一种瑞司美替罗新晶型及其制备方法
WO2026067708A1 (fr) * 2024-09-30 2026-04-02 齐鲁制药有限公司 Formes cristallines de resmétirom, son procédé de préparation et son utilisation
WO2026074443A1 (fr) 2024-10-01 2026-04-09 Assia Chemical Industries Ltd. Formes solides de resmétirom
CN119306670A (zh) * 2024-10-12 2025-01-14 北京海美桐医药科技有限公司 瑞司美替罗中间体、其合成方法和瑞司美替罗的合成方法

Family Cites Families (19)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPS5615272A (en) * 1979-07-17 1981-02-14 Ishihara Sangyo Kaisha Ltd N-benzoyl-n'-phenylurea compound, its preparation, and insecticide containing the same
GB0028429D0 (en) 2000-11-22 2001-01-10 Astrazeneca Ab Therapy
MXPA05008080A (es) * 2003-01-28 2006-02-08 Octoplus Technologies B V Inhibidores peptidicos de toxinas derivadas de la ll-37.
CN100469769C (zh) 2003-03-24 2009-03-18 弗·哈夫曼-拉罗切有限公司 作为逆转录酶抑制剂的苄基-哒嗪酮
ITRM20030363A1 (it) 2003-07-24 2005-01-25 Fernando Goglia Composizioni comprendenti la 3, 5diiodotironina e uso farmaceutico di esse.
US20080152700A1 (en) * 2004-06-01 2008-06-26 Reza Sheikhnejad Methods and compositions for the inhibition of gene expression
US7807647B2 (en) * 2004-06-01 2010-10-05 Pronai Therapeutics, Inc. Methods and compositions for cancer therapy
CA2589106C (fr) 2004-11-02 2015-07-21 Northwestern University Composes pyridazine, compositions et procedes associes et leur utilisation dans le traitement de maladies inflammatoires
DK1919878T3 (da) * 2005-07-21 2010-10-25 Hoffmann La Roche Pyridazinonderivater som thyroidhormonreceptoragonister
HRP20100611T1 (hr) * 2007-06-06 2010-12-31 Torrent Pharmaceuticals Ltd Novi spojevi
US8076334B2 (en) * 2007-09-20 2011-12-13 Hoffmann-La Roche Inc. Prodrugs of thyroid hormone analogs
AR092872A1 (es) * 2012-09-17 2015-05-06 Madrigal Pharmaceuticals Inc Metodo para sintetizar analogos de la hormona tiroidea y polimorfos de los mismos
US8858502B2 (en) 2012-10-10 2014-10-14 Alcon Research, Ltd. Systems and methods for external pressure sensing
CN106132969A (zh) 2014-02-14 2016-11-16 森普拉制药公司 用于治疗糖尿病和肝病的组合物和方法
WO2018075650A1 (fr) 2016-10-18 2018-04-26 Madrigal Pharmaceuticals, Inc. Méthodes de traitement de troubles hépatiques ou de troubles lipidiques avec un agoniste thr-bêta
ES3029158T3 (en) 2018-06-12 2025-06-23 Xizang Haisco Pharmaceutical Co Ltd Thyroid hormone receptor agonists and uses thereof
AR115666A1 (es) 2018-07-02 2021-02-10 Madrigal Pharmaceuticals Inc Formas sólidas de 2-(3,5-dicloro-4-((5-isopropil-6-oxo-1,6-dihidropiridazin-3-il)oxi)fenil)-3,5-dioxo-2,3,4,5-tetrahidro-1,2,4-triazin-6-carbonitrilo
CA3113373A1 (fr) 2018-10-12 2020-04-16 InventisBio Co., Ltd. Agonistes du recepteur des hormones thyroidiennes
CN111320609A (zh) 2018-12-13 2020-06-23 拓臻股份有限公司 一种THRβ受体激动剂化合物及其制备方法和用途

Also Published As

Publication number Publication date
IL320269A (en) 2025-06-01
EP2895466B1 (fr) 2020-03-25
EP4406594A2 (fr) 2024-07-31
IN2015DN03133A (fr) 2015-10-02
JP2019048856A (ja) 2019-03-28
EP4023641A3 (fr) 2022-09-14
CA3090070C (fr) 2023-01-24
RU2015114327A (ru) 2016-11-10
LT4406594T (lt) 2025-12-29
NZ739645A (en) 2019-11-29
CN108101851A (zh) 2018-06-01
EP4023641B1 (fr) 2024-05-01
NO2026010I1 (no) 2026-03-03
RU2668960C2 (ru) 2018-10-05
IL275393B (en) 2022-01-01
US20160243126A1 (en) 2016-08-25
FIC20265007I1 (fi) 2026-03-03
IL275393A (en) 2020-07-30
JP6532931B2 (ja) 2019-06-19
NZ705827A (en) 2018-07-27
EP3689853B1 (fr) 2021-11-24
AU2013315017A1 (en) 2015-04-02
DK3689853T3 (da) 2022-03-07
ES2795450T3 (es) 2020-11-23
IL314360B1 (en) 2025-05-01
US20240122936A1 (en) 2024-04-18
US20240148742A1 (en) 2024-05-09
AR092872A1 (es) 2015-05-06
DK2895466T3 (da) 2020-06-08
JP2020015739A (ja) 2020-01-30
US9266861B2 (en) 2016-02-23
TWI652260B (zh) 2019-03-01
ZA201501795B (en) 2021-10-27
JP6616688B2 (ja) 2019-12-04
JP6899413B2 (ja) 2021-07-07
PT4406594T (pt) 2025-11-28
KR102138750B1 (ko) 2020-07-29
NL301369I2 (nl) 2026-03-30
US10894050B2 (en) 2021-01-19
IL259610A (en) 2018-07-31
IL288133A (en) 2022-01-01
KR20150056630A (ko) 2015-05-26
JP2025179154A (ja) 2025-12-09
JP2020109090A (ja) 2020-07-16
EP3689853A1 (fr) 2020-08-05
JP7436542B2 (ja) 2024-02-21
EP2895466A4 (fr) 2016-08-10
EP4691557A2 (fr) 2026-02-11
US9968612B2 (en) 2018-05-15
SG10201705984XA (en) 2017-08-30
IL288133B1 (en) 2024-08-01
RS67728B1 (sr) 2026-03-31
MX2018014924A (es) 2020-09-02
US20210161904A1 (en) 2021-06-03
US11986481B2 (en) 2024-05-21
KR20180131647A (ko) 2018-12-10
WO2014043706A1 (fr) 2014-03-20
EP2895466A1 (fr) 2015-07-22
BR112015005891A2 (pt) 2017-08-08
IL259610B (en) 2020-06-30
AU2013315017C1 (en) 2017-11-23
TWI755628B (zh) 2022-02-21
EP4691557A3 (fr) 2026-03-18
MX2015003418A (es) 2016-04-04
SG10202006058QA (en) 2020-08-28
TW201946917A (zh) 2019-12-16
CN105008335B (zh) 2018-12-21
HK1212682A1 (en) 2016-06-17
EP4406594A3 (fr) 2024-11-06
IL237628B (en) 2019-07-31
US20150203473A1 (en) 2015-07-23
JP6765408B2 (ja) 2020-10-07
EP4406594B1 (fr) 2025-09-10
US10376517B2 (en) 2019-08-13
KR102363776B1 (ko) 2022-02-15
EP4023641A2 (fr) 2022-07-06
IL265030B (en) 2020-07-30
KR20210083381A (ko) 2021-07-06
KR101966490B1 (ko) 2019-08-14
MY170520A (en) 2019-08-08
TWI804870B (zh) 2023-06-11
FI4406594T3 (fi) 2025-11-26
RU2018128393A3 (fr) 2019-04-16
US20190381053A1 (en) 2019-12-19
PL4406594T3 (pl) 2026-03-30
IL314360A (en) 2024-09-01
TW202134217A (zh) 2021-09-16
CA3090070A1 (fr) 2014-03-20
US11564926B2 (en) 2023-01-31
SG11201501907YA (en) 2015-04-29
JP2024056793A (ja) 2024-04-23
HRP20251398T1 (hr) 2026-03-13
RU2018128393A (ru) 2019-03-14
JP7038745B2 (ja) 2022-03-18
TW201425300A (zh) 2014-07-01
JP2018080188A (ja) 2018-05-24
US20230210856A1 (en) 2023-07-06
ES2907926T3 (es) 2022-04-27
JP2015535817A (ja) 2015-12-17
LTPA2026507I1 (fr) 2026-03-10
TWI681957B (zh) 2020-01-11
IL314360B2 (en) 2025-09-01
IL237628A0 (en) 2015-04-30
MX395148B (es) 2025-03-24
AU2013315017B2 (en) 2017-07-27
FR26C1009I1 (fr) 2026-04-17
IL288133B2 (en) 2024-12-01
DK4406594T3 (da) 2025-11-03
CA2884481C (fr) 2021-04-27
SI4406594T1 (sl) 2026-03-31
JP2022078218A (ja) 2022-05-24
BR122021024202B1 (pt) 2022-05-17
CA3111317A1 (fr) 2014-03-20
ES3053122T3 (en) 2026-01-19
CA3111317C (fr) 2023-08-29
CA2884481A1 (fr) 2014-03-20
MX364661B (es) 2019-05-03
US20180228807A1 (en) 2018-08-16
TW201906835A (zh) 2019-02-16
KR20200023528A (ko) 2020-03-04
CN105008335A (zh) 2015-10-28

Similar Documents

Publication Publication Date Title
WO2014043706A8 (fr) Procédé de synthèse d'analogues de l'hormone thyroïdienne et de ses polymorphes
JOP20210065A1 (ar) عملية لتحضير 5- فلورو-1h- بيرازولوبيريدينات مستبدلة
WO2011123668A3 (fr) Synthèse stéréosélective d'agents actifs contenant du phosphore
WO2012031045A3 (fr) Dérivés esters phosphonates et leurs procédés de synthèse
NZ734535A (en) Process of producing cycloalkylcarboxamido-indole compounds
MY159252A (en) Process for the preparation of dopo-derived compounds and compositions thereof
WO2014041559A3 (fr) Procédé de préparation d'étéxilate de dabigatran et ses intermédiaires
PH12012501438A1 (en) Method for preparing tetrazole methanesulfonic acid salts, and novel compound used in same
MX377644B (es) 6.7.beta-epóxidos esteroideos como intermedios químicos.
MY178759A (en) Method for preparing trichlorosilane
MD20120129A2 (en) Process for the preparation of perindopril L-arginine salt
EA201300647A1 (ru) Оптимизированный синтез чистых неполиморфных кристаллических жёлчных кислот с заданным размером частиц
BR112012031086A2 (pt) intermediários de agomelatina e método de preparação dos mesmos
WO2011102640A3 (fr) Procédé de préparation de sitagliptine et sels d'amines intermédiaires utilisés dans ce procédé
PH12013500609A1 (en) Novel method of preparing benzoimidazole derivatives
WO2012115402A3 (fr) Forme cristalline du docétaxel et procédé de préparation associé
MX349752B (es) Proceso para la preparacion de 3-metilsulfonilpropionitrilo.
MX338556B (es) Metodos para aislar acidos 4-cloro-2-fluoro-3-fenilboronicos sustituidos.
CA2928305C (fr) Forme anhydre cristalline du cabazitaxel, son procede de preparation et ses compositions pharmaceutiques
WO2012052939A3 (fr) Préparation de composés de bicyclo[2.2.2]octan-2-one
WO2011154586A3 (fr) Procédés améliorés pour la préparation de dérivés de quinoxaline
MX2013010009A (es) Metodo de radiofluoracion.
WO2010086700A3 (fr) Procédé amélioré de préparation du sel cholinique de l'acide fénofibrique et polymorphe inédit de celui-ci
IN2012DE00267A (fr)
TH1101002691A (th) กระบวนการสังเคราะห์ เอทธินิล เอสทราไดออลจากสารตั้งต้นโซลาโซดีน

Legal Events

Date Code Title Description
121 Ep: the epo has been informed by wipo that ep was designated in this application

Ref document number: 13837402

Country of ref document: EP

Kind code of ref document: A1

WWE Wipo information: entry into national phase

Ref document number: 237628

Country of ref document: IL

ENP Entry into the national phase

Ref document number: 2884481

Country of ref document: CA

ENP Entry into the national phase

Ref document number: 2015532148

Country of ref document: JP

Kind code of ref document: A

NENP Non-entry into the national phase

Ref country code: DE

WWE Wipo information: entry into national phase

Ref document number: MX/A/2015/003418

Country of ref document: MX

ENP Entry into the national phase

Ref document number: 2013315017

Country of ref document: AU

Date of ref document: 20130917

Kind code of ref document: A

WWE Wipo information: entry into national phase

Ref document number: 2013837402

Country of ref document: EP

REG Reference to national code

Ref country code: BR

Ref legal event code: B01A

Ref document number: 112015005891

Country of ref document: BR

ENP Entry into the national phase

Ref document number: 20157009807

Country of ref document: KR

Kind code of ref document: A

ENP Entry into the national phase

Ref document number: 2015114327

Country of ref document: RU

Kind code of ref document: A

ENP Entry into the national phase

Ref document number: 112015005891

Country of ref document: BR

Kind code of ref document: A2

Effective date: 20150317

WWD Wipo information: divisional of initial pct application

Ref document number: 320269

Country of ref document: IL